[EN] SUBSTITUTED AZABICYCLO HEXANE DERIVATIVES AS MUSCARINIC RECEPTOR ANTAGONISTS<br/>[FR] DERIVES D'AZABICYCLO HEXANES SUBSTITUES EN TANT QU'ANTAGONISTES DES RECEPTEURS MUSCARINIQUES
申请人:RANBAXY LAB LTD
公开号:WO2004089363A1
公开(公告)日:2004-10-21
This invention generally relates to derivatives of substituted azabicyclo hexanes of formula I. The compounds of this invention can function as muscarinic receptor antagonists, and can be used for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to a process for the preparation of the compounds of the present invention, pharmaceutical compositions containing the compounds of the present invention and the methods of treating the diseases mediated through muscarinic receptors.
Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4
作者:Mui Cheung、Weike Bao、David J. Behm、Carl A. Brooks、Michael J. Bury、Sarah E. Dowdell、Hilary S. Eidam、Ryan M. Fox、Krista B. Goodman、Dennis A. Holt、Dennis Lee、Theresa J. Roethke、Robert N. Willette、Xiaoping Xu、Guosen Ye、Kevin S. Thorneloe
DOI:10.1021/acsmedchemlett.7b00094
日期:2017.5.11
failure. Herein we report the discovery of an orallyactive, potent, and selective TRPV4 blocker, 3-(1,4'-bipiperidin-1'-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide (GSK2193874, 28) after addressing an unexpected off-target cardiovascular liability observed from in vivo studies. GSK2193874 is a selective tool for elucidating TRPV4 biology both in vitro
[EN] 6-PHENYL- OR 6-(PYRIDIN-3-YL)INDAZOLE DERIVATIVES AND METHODS OF USE<br/>[FR] DÉRIVÉS DE 6-PHÉNYL OU 6-(PYRIDIN-3-YL)INDAZOLE ET PROCÉDÉS D'UTILISATION
申请人:ABBVIE INC
公开号:WO2015112445A1
公开(公告)日:2015-07-30
Compounds of formula (I) and pharmaceutically acceptable salts, esters, amides, or radiolabelled forms thereof, wherein R1, R2, R3, R4, R5, R6, and X are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by Tropomysin receptor kinases (Trk). Methods for making the compounds are disclosed. Also disclosed are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.
6 Phenyl or 6 Pyridin 3 YL Indazole Derivatives and Methods of Use
申请人:ABBVIE INC.
公开号:US20160376240A1
公开(公告)日:2016-12-29
Compounds of formula (I) and pharmaceutically acceptable salts, esters, amides, or radiolabelled forms thereof, wherein R
1
, R
2
, R
3
, R
4
, R
5
, R
6
, and X are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by Tropomysin receptor kinases (Trk). Methods for making the compounds are disclosed. Also disclosed are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.
New carboxamide compounds having melanin concentrating hormone antagonistic activity, pharmaceutical preparations comprising these compounds and process for their manufacture
申请人:Boehringer Ingelheim International GmbH
公开号:US20040242572A1
公开(公告)日:2004-12-02
The present invention relates to carboxamide compounds of general formula I
1
wherein the groups and residues A, B, W, X, Y, Z, R
1
, R
2
, R
3
and k have the meanings given in claim 1. Moreover the invention relates to process for preparing the above mentioned carboxamides as well as pharmaceutical compositions containing at least one carboxamide according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.